Anti-inflammatory painkillers are a genre of medicines that can be utilized to alleviate pains, sprains, strains and other common effects of arthritis. They can be consumed orally in the form of tablets, liquids or capsules, injected via needle, or applied to skin in the form of a topical gel or cream. The mechanisms of action of either of these when used as anti-inflammatories is varied.
When applied to skin in the form of a topical preparation, the anti-inflammatory painkillers are sometimes called topical non-steroidal anti-inflammatory drugs (NSAIDs) or just topical anti-inflammatories as a generic term. The NSAIDs are often prescribed as a preliminary treatment for mild to moderate musculoskeletal pain, sprains, strains, and arthritis. High plasma concentrations of oral NSAIDs are required to achieve effective tissue concentrations at the site of pain and inflammation.
In an attempt to find relief of musculoskeletal pain with NSAIDs, topical application NSAID's have been developed to deliver adequate local tissue concentrations with minimal systematic absorption. It has been found that plasma concentrations following topical administration of NSAIDs gels are far lower than levels found after oral administration.
NSAIDs work in the same way as oral anti-inflammatory painkillers, in which the oral anti-inflammatories when taken my mouth, work to inhibit or block the effect of chemicals called cyclo-oxygenase (COX) enzymes. COX enzymes typically aid in the production of prostaglandins, some of which assist in the production of pain and inflammation at site. A reduction in prostaglandin production means lesser pain and inflammation. NSAIDs specifically work only on the area that the topical gel has been applied to rather than the entire body like their oral painkiller counterparts. When topically applied, the NSAIDs are absorbed into the skin of the user and move deeper into the areas of the body like the muscle itself, where there is pain and inflammation exists at site. Using NSAIDs in the form of topical preparation can mean that the total amount of anti-inflammatory in the user's body is very low. This could also mean that that the user is less likely to encounter any potential side-effects due to such use.
However, the effectiveness of topical NSAIDs for the treatment of acute back pain or chronic conditions including chronic back pain is still unknown. Several systematic reviews report trials of poor quality with most trial lengths lasting less than four weeks and demonstrating inconclusive results. Trials comparing oral NSAIDs and their topical equivalents show conflicting results with regards to efficacy. There is insufficient data to perform any thorough meta-analysis. Furthermore, there are not many published results about the effects of NSAIDs in patient populations commonly seen in palliative care settings. Research shows no benefit from a topical NSAIDs cream over placebo in the relief of related pain. Given the expense of topical NSAIDs unclear benefit over prolonged time periods and unknown efficacy compared to oral preparations, they are generally not recommended for chronic musculoskeletal pain.
NSAIDs used regularly for sports injuries, painful joints and arthritis are effective to treat inflammation, however they present skin side effects that can become severe in some people. The topical diclofenac gel has presented allergic contact dermatitis, dryness (irritant dermatitis) and scaling. Also the use of topical NSAID gels or creams to treat pain has been reported to cause a photocontact dermatitis. It has been observed that the reaction appears after stopping the application where the skin is exposed to sunlight. It has also been observed that NSAID gels can produce exanthema, itch, morbilliform, rash, photosensitivity, urticaria and angioedema.
On the other hand, while topical steroids have important benefit in reducing inflammation, they also have significant side effects. Most of the side-effects are seen in long-term use, but some may also be seen within days of starting such a therapy. Side effects consist of: 1) skin atrophy, which causes the thinning of the epidermis and changes in the connective tissue of the dermis, wrinkled skin, hypopigmentation and prominence of underlying veins, 2) alteration in immune function, which can inhibit the skin's ability to fight off bacterial or fungal infections, 3) tachyphylaxis, the tolerance the skin develops to the vaso-constrictive action of topical steroids, 4) steroid rosacea, which is redness and pustules as commonly observed in fair skinned people, 5) topical steroid allergy, which has been observed in 4 to 5 percent of people who use topical steroids, 6) stretch marks in areas where the skin touches skin such as groin and armpits, most of which are itchy, permanent and irreversible, 7) immune-suppression, which is caused when topical steroids are used to skin infection of fungal origin causing the user to get a rash that gets redder, itchier and spreads more extensively than a typical fungal infection. As a result, there is a widespread pustular inflammation called tinea incognito.
Therefore, a need exists to overcome the problems with the prior art as discussed above, and particularly for a more efficient way of providing an anti-inflammatory and analgesic composition.